Synthesis and biological evaluation of benzothiazole ...



Title Synthesis and biological evaluation of benzothiazole derivatives of pyrimidines, acrylonitriles, and coumarins.
Author(s) Amal M. Youssef, Hany M. Mohamed, Caitlin Czezowski, Athar Ata, Alaa S. Abd-El-Aziz
Journal Heterocycles,
Date 2006
Volume 68
Issue 2
Start page 347
End page 355
Abstract A number of benzothiazole derivatives of 2-aminopyrimidines (3a-b, 5, 6a-b, and 7), benzothiazole-3-arylacrylonitriles (10a-c), and benzothiazol-2-yl-coumarins (18a c, and 20) were synthesized by reacting benzothiazole derivatives with dicarbonyl compounds, and aromatic aldehydes. The unexpected 2-(4-methoxyphenyl)benzo[d]thiazole (14) was obtained as a unique product via the reaction of 2-aminothiophenol with ethyl 3-(4-methoxyphenyl)-2-scyanoacrylate. 2-(Benzo[d]thiazol-2-yl)-3-(4-hydroxyphenyl)acrylonitrile (10a) exhibited activity against Staphylococcus aureus. 2-(Benzo[d]thiazol-2-ylamino)pyrimidine-4,6-(1H,5H)-dione (3b) showed antibacterial activity selectivity against Corynebacterium xerosis. 2-(Benzo[d]thiazol-2-ylamino)-6-methylpyrimidin-4(3H)-one (5) showed weak anti-fungal activity against Candida albicans.
DOI 10.3987/COM-05-10609

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